MICRODIALYSIS AND PHARMACOKINETIC STUDY OF TR-701

这个子项目是许多研究子项目中的一个 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可以在其他CRISP条目中表示。所列机构为 研究中心，而研究中心不一定是研究者的研究机构。 TR-701是一种恶唑烷酮抗生素，是微生物活性分子TR-700的前药。 TR-700对药物敏感和耐药革兰氏阳性菌和一些革兰氏阴性菌（如嗜肺军团菌和抗酸细菌结核分枝杆菌）具有活性。 由于该化合物的适应症之一是复杂的皮肤和皮肤结构感染，因此了解感染部位的药物浓度非常重要。 这包括皮下脂肪组织和骨骼肌。 然而，传统上，由于缺乏适当的方法来测量这些部位的浓度，因此采集血浆样本来检查药效学反应。 FDA和其他监管机构一直建议公司更深入地研究药代动力学/药效学关系，以开发最佳给药方案。 为此，必须知道靶部位的药物浓度。 最近，一种新的采样技术已成为有用的测量药物浓度在几乎每一个组织，微透析。 本研究的目的是使用微透析技术来检查与血浆样品相比，TR-701单次口服给药后的软组织浓度。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. TR-701, an oxazolidinone antibiotic, is a prodrug of the microbiologically-active molecule, TR-700. TR-700 has activity against drug-susceptible and drug-resistant Gram-positive bacteria, and some Gram-negative bacteria such as Legionella pneumophila and the acid-fast bacterium Mycobacterium tuberculosis. Since one of the indications for this compound is complicated skin and skin structure infections, it is important to know the concentration of the drug at the site of infection. This includes subcutaneous adipose tissue and skeletal muscle. Traditionally, however, for lack of an appropriate method to measure the concentration at these sites, plasma samples have been taken to examine the pharmacodynamic response. The FDA and other regulatory agencies have been recommending that companies examine pharmacokinetic/pharmacodynamic relationships more intensely to develop optimal dosing regimens. To do so, the drug concentrations at the target site must be known. Recently, a new sampling technique has become useful in measuring drug concentrations in virtually every tissue, microdialysis. The aim of this study is to use the microdialysis technique to examine the soft tissue concentrations after a single oral dose of TR-701 compared to plasma samples.